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Pharmaceutics II Exam 2 > Topical preparations - suppositories > Flashcards

Topical preparations - suppositories Flashcards

1
Q

what type of suppositories are available

A

rectal
vaginal
urethral

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2
Q

define suppositories

A

suppositories are solid dosage forms intended for insertion into body orifices where they MELT, SOFTEN, OR DISSOLVE and exert localized OR systemic effects

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3
Q

true or false

suppositories are solid dosage forms and only provide systemic effects

A

false

they are solid dosage forms but can provide local or systemic effects

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4
Q

explain the shape, length, and mass of rectal suppositories

A

cylindrical shape
~32mm in length
~2 grams* (NO MORE THAN 2 GRAMS)

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5
Q

Explain the shape and mass of vaginal suppositories

A

pessaries, globular or cone shaped
~5 grams

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6
Q

explain the shape and mass of urethral suppositories

A

slender, pencil shaped
~4 grams

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7
Q

explain the action of local suppositories

A

the suppository base melts, softens, or dissolves and delivers the medication to the tissues of that local region

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8
Q

name 4 things in which the local action of suppositories can provide relief

A

pain
irritation
itching
inflammation

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9
Q

explain what hemorroidal suppositories are.
do they provide local or systemic effects?

A

local effects

they are local anesthetics, vasoconstrictors, astringents, analgesics, soothing emollients, and protective agents

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10
Q

what can vaginal suppositories be used for

A

contraceptives and antiseptics

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11
Q

give an example of a vaginal contraceptive and how it works

A

nonxynol-9

is a surfactant that can interact with the cell membrane and be a barrier

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12
Q

what LOCAL action can urethral suppositories have

A

antibacterials and local anesthetics

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13
Q

which type of suppositories can be used for systemic effects and why?

A

rectal and vaginal, because many drugs can be absorbed through the mucous membranes in those areas

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14
Q

name 5 advantages that systemic suppositories have over the oral route

A

-effective route for patients who have vomiting issues

-convenient route for patients or are unable or unwilling to swallow medication

-bypass hepatic first pass metabolism

-a drug that is irritating to the stomach when given orally can be given via suppository and not cause this irritation

-avoids GI incompatibility of drugs (inactivation of drugs by the pH or enzymatic activity of the stomach)

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15
Q

which have more options available to provide systemic effects – ointments, creams, or suppositories?

A

suppositories have the most

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16
Q

what is the length of the human rectum

A

15-30cm

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17
Q

how many mL of insert fluid is available for the human rectum

A

2-3mL

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18
Q

true or false

there are villi and microvilli present in the human rectum

A

FALSE – there is not

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19
Q

speak about the vascularization of the human rectum

A

there is abundant blood vascularization and lymphatic vessels

the lower hemorrhoidal veins that surround the colon receive the absorbed drug and initiate circulation throughout the body, BYPASSING THE LIVER (not 100%)
lymphatic circulation assists in the absorption

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20
Q

true or false

in the case of drug absorption from rectal suppositories, first pass effects are 100% avoided

A

FALSE

the lower hemorrhoidal veins that surround the colon receive the absorbed drug and initiate circulation throughout the body which bypasses the liver, BUT the upper region of the rectum may absorb some drug as well and go to the hepatic vein

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21
Q

what assists in drug absorption from rectal suppositories

A

lymphatic circulation

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22
Q

explain the pH and buffer capacity of the human rectum

A

the pH of the rectal fluid is around 7-8 and has NO buffer capacity

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23
Q

the pH of the human rectum is 7-8 (about neutral)
what is the benefit of this?

A

don’t have to worry about an acid-base reaction occurring and the drug is generally NOT chemically changed in the rectal environment

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24
Q

explain how colonic contents (contents of the colon) can affect drug absorption through the rectum

A

a void (empty) rectum provides greater absorption

diarrhea and colonic obstruction due to a tumor will lessen absorption

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25
Q

what physiochemical factors must be considered with drug absorption from the rectum

A

the lipid-water solubility and the particle size

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26
Q

why is particle size a physiochemical factor to consider when considering drug absorption from rectal suppositories

A

the partition coefficient

a lipophilic drug in a fatty suppository base at a low concentration will have less tendency to escape from the base and will result in LOW bioavailability because the majority of the drug will remain in the suppositiry

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27
Q

why is particle size a concern when considering the absorption of drugs from rectal suppositories

A

the smaller the particle size, the more readily available the drug is for absorption

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28
Q

true or false

when considering rectal suppositories, it is not ideal to have the drug be very soluble in the base because the drug won’t release much and bioavailability will be low

A

TRUE

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29
Q

Classify the suppository bases

A

-fatty or oleaginous
-water soluble or water miscible
-miscellaneous

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30
Q

explain the ideal suppository base

A

-bland and non irritating, chemically stable, compatible with the med, easily forms a solid by compressing or molding, remains a solid at room temp but softens, melts, or dissolves readily at body temp

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31
Q

true or false

a strong drug-base interaction inhibits the release of the drug

A

TRUE

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32
Q

why must a suppository base be capable of melting, softening, or dissolving?

A

to release the medication

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33
Q

for which are we more concerned with irritation - suppositories or ointments?

A

suppositories bc the tissues where they’re inserted are very sensitive

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34
Q

what are the most frequently used suppository bases

A

fatty or oleaginous bases (hydrocarbons)

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35
Q

give 5 examples of fatty/oleaginous suppository bases.
which is the most popular

A

cocoa butter**
palm kernel oil
cottonseed oil
glyceryl monostearate
glyceryl monopalmitate

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36
Q

explain all of the properties of cocoa butter.
include:

-where is it obtained from
-what color and state of matter
-what chemical structure
-what temp does it melt
-what solidifying agents are included

A

natural product obtained from Theobroma Cacao

yellowish-white solid

chemically – a triglyceride

melts at 30-36 degrees C

solidfiying agents: cetyl esters wax (beeswax)

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37
Q

true or false

cocoa butter contains water

A

FALSE - does not contain water. it is a triglyceride that contains fatty acid groups

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38
Q

what is a disadvantage of cocoa butter that sometimes causes us to use PEG instead

A

it melts at 30-36 degrees celsius which is around our body temperature.
thus, if we hold it for too long it’ll start to get soft

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39
Q

give 5 advantages of PEG bases

A

-do not need to be formulated to melt at body temp

-its melting point is considerably higher than body temp. convenient for storage – does not need fridge

-PEG bases permit slow release of the drug

-easy to handle when administering

-do not leak from the orifice (like many cocoa butter base suppositories)

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40
Q

name the water-soluble/water miscible suppository bases that are available in the market

A

glycerinated gelatin and PEG bases (carbowax)

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41
Q

true or false

water soluble/water miscible suppository bases do NOT contain water

A

TRUE

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42
Q

which is more popular as a water soluble/water miscible suppository base - glycerinated gelatin or PEG bases

A

PEG is more popular

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43
Q

explain PEG suppository bases (carbowax)

A

mix PEG 200-600 (clear liquid) with PEG 1000 or more (wax-like, white solid) to get the desired consistency

PEG 200, 400, 600, 1000, 1500, 1540, 3350, 4000, 6000, AND 8000 are used

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44
Q

explain how PEG bases are used and how they are formed

A

they do not melt at body temp (like cocoa butter), they dissolve slowly in the body fluids. this allows for controlled release for a prolonged period of time/

formed via FUSION METHOD (uses heat)

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45
Q

explain why glycerinated gelatin water soluble/water miscible base contains the ingredients it does

A

gelatin is also a component of capsules.
glycerin is added to soften the gelatin

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46
Q

true or false

ointment bases cannot be used for suppository bases

A

false - a lot can

47
Q

true or false

suppository bases do not contain water

A

true

48
Q

explain the difference in storage between cocoa butter and PEG

A

cocoa butter must be stored in the fridge because it softens at room tmep, but PEG does not

49
Q

true or false

miscelaneous suppository bases are normally not used

A

true

50
Q

name some formulation variables for suppository based

A

physical state
particle size
solubility
viscosity
brittleness
volume contraction
drug release rates
special problems

51
Q

what can the physical state of the API of the suppository base be?

A

can be liquid or powder

52
Q

of the formulation variables for suppository bases, which are related to the drug itself ?

A

physical state
particle size
solubility

53
Q

small particle size = ____solubility and ____ bioavailability

A

high solubility and high bioavailability

54
Q

what are some things to consider if the drug used in the suppository are solid particles?

A

need to use levitation to sufficiently reduce the particle size

55
Q

what is aspirin solubility in PEG base? what does this mean?

A

aspirin solubility in PEG base is LOW
therefore, a little of the drug will dissolve in the PEG base and the insoluble particles will be dispersed in the base.

THIS IS HOW THE RELEASE RATE IS CONTROLLED

56
Q

how is solubility a concern when formulating suppositories

A

the solubility of the drug in the base used — helps to control the release rate

57
Q

explain the ideal “brittleness” of the suppository base

A

it cannot be easily broken. we want to maintain ridgedness to a certain extent but not break it when inserted

58
Q

explain the release rate of:

oil-soluble drug in an oily base

A

slow release bc of poor escaping tendency

this will provide long duration

59
Q

explain the drug release rate of:

water soluble drug in an oily base

A

this will provide RAPID RELEASE

the solubility is bad so some drug dissolves but not a lot. thus, only a small quantity of drug is needed.

60
Q

is this acceptable:

solubility of the drug is 10mg in 100g.
solubility of the drug in the base is very bad.
1 mg will provide therapeutic effect

A

YES it is okay. most of the drug will be able to release out because solubility is so poor

61
Q

explain the drug release rate of:

oil soluble drug in water muscle base (PEG)

A

MODERATE RELEASE

62
Q

explain the drug release rate of:

water miscible drug in water miscible base

A

moderate release — all based on diffusion

all are water soluble

63
Q

true or false

when a drug dissolves in the suppository base, it can easily escape to provide therapeutic effect

A

FALSE

the drug will remain there and not come out

the INSOLUBLE PARTICLES are the ones that are able to escape

64
Q

true or false

suppositories can only contain solid/powder API

A

false

can contain liquid API as welll

65
Q

how is “volume contraction” a formulation consideration when preparing suppositories?

A

in the molding method, when the suppository is placed in the fridge some of the material changes

the amount that changed depends on the drug and how much base we use

66
Q

true or false

for both suppositories and ointments, the amount of drug incorporated is usually low

A

true

67
Q

true or false

drug release rates only apply to suppositories

A

FALSE

applies to ointments and suppositories

68
Q

how many methods are there for preparation of suppositories? name them

A

3:
molding
hand rolling and shaping
compression

69
Q

explain the molding method of preparing suppositories

A

the base is melted. the melt is incorporated into the molds. allow the melt to cool and congeal (harden) into suppositories. remove the formed suppositories from the mold

the mold must be lubricated to prevent sticking, and calibrated

determining the amount of base required is challenging

preparing and pouring the melt

70
Q

name a lubricant for suppository molds

A

liquid petrolatum (mineral oil)

71
Q

if you use a HIGH DENSITY DRUG, the volume occupied will be _____

what does this say about the amount of base needed

A

LOW
therefore, a lot of base will be needed

72
Q

which suppository base(s) can use hand rolling/shaping as a method of preparation?

A

ONLY for cocoa butter - not PEG. PEG is not soft enough to be able to do this and needs to be melted

73
Q

what 2 ingredients require the use of a lubricant in the molding method?

A

glycerin and gelatin

74
Q

which suppository base has the more significant volume constriction problem ?

A

PEG

when it shrinks, it won’t stick to the mold

75
Q

the compression method of preparing suppositories is mainly used where?

A

in manufacturing

76
Q

explain the compression method of preparing suppositories.
where is it mainly used?

A

prepared by forcing the mixed mass of the suppository based and medicaments into special molds using suppository making machines

suppository base + medicaments + other ingredients undergo thorough mixing prior to this compression

THE COMPRESSION PROCESS IS SUITABLE FOR WHAT KIND OF COMPONENTS
-heat labile (sensitive)
-suppositories containing a great deal of insoluble substances in the base

77
Q

what suppository bases are suitable for the molding method

A

cocoa butter
glycerinated gelatin
PEG
most other bases too

78
Q

true or false

basically any suppository base can use the molding method

A

TRUE

79
Q

what kind of components/bases are suitable for the compression method of preparing suppositories ?

A

heat sensitive components and suppositories containing a lot of insoluble substances

80
Q

true or false

hand rolling/shaping CANNOT be used for cocoa butter bases

A

FALSE

can be used for cocoa butter but not PEG because it isn’t soft enough

81
Q

name 3 stability concerns for suppositories

A

physical stability
chemical stability
microbiological stability

82
Q

explain microbiological stability for suppositories

A

-for COMPOUNDED suppositories - beyond use dating

-for MANUFACTURED suppositories - expiration dating

-inform and education the patient about storage - if PEG, room temp is fine. cocoa butter needs fridge.

glycerin has evaporating issue — needs to be stored properly otherwise it will become brittle when evaporates

83
Q

explain how a suppository should be inserted

A

-position patient on left side with upper leg flexed. lubricate the suppository with a water soluble lubricant (or small amount water) if needed.

gently insert suppository a finger length deep at an angle towards umbilicus so the suppository is placed against the rectal wall for ABSORPTION, rather than being left in the canal or pushed into mass of stool

after the finger is withdrawn, hold buttocks together until urge to expel has ceased

84
Q

low particle size = _____ sedimentation

A

slow

85
Q

low viscosity of the suspension = _____ sedimentation

A

high

86
Q

true or false

the addition of a flocculating agent will increase the sedimentation rate

A

true

87
Q

true or false

increasing the particle size of the active ingredient will decrease sedimentation rate

A

false - increase

88
Q

true or false

particles in flocculated suspensions exist as separate entities

A

FALSE - deflocculated

89
Q

is the sedimentation rate high in flocculated or deflocculated suspensions?

A

flocculated

90
Q

true or false

talc can be used as a suspending agent

A

false

91
Q

name 2 suspending agents

A

acacia
methylcellulose

92
Q

name 2 advantages of aerosol dosage forms

A

fine particle size
less contamination

93
Q

true or false

aerosol dosage forms are relatively inexpensive to make

A

false - expensive

94
Q

propellants used in aerosols have ___ vapor pressure at 70 degrees fahrenheit

A

high

95
Q

what does high vapor pressure mean

A

they easily evaporate

96
Q

true or false

propellants used in aerosols may not dissolve in water

A

TRUE

97
Q

true or false

the propellants used in aerosols have liquid densities LOWER than water at 70 degrees fahrenheit

A

true

98
Q

substances used as suppository bases that DISSOLVE rather than melt…

A

any PEG

99
Q

true or false

water soluble bases do not contain aqueous solution

A

TRUE

100
Q

true or false

absorption bases contain aqueous solution

A

true — when anhydrous becomes W/O emulsions

101
Q

true or false

hydrocarbon bases can be used for preparation of W/O emulsions

A

false

102
Q

true or false

absorption bases can be used for preparation of W/O emulsions

A

true

103
Q

true or false

water removable bases can be used for preparation of W/O emulsions

A

FALSE

104
Q

can an aqueous solution be incorporated into white petrolatum?

A

no - it is hydrocarbon base

105
Q

can aqueous solution be incorporated into vaseline?

A

NO - hydrocarbon

106
Q

true or false

lanolin can be used to incorporate aqueous solutions

A

yes — it is an absorption base

107
Q

nitroglycerin TDDS can be compared on the basis of?

A

the number of mg of nitroglycerin delivered in 24 hours

daily delivery amount

108
Q

true or false

Nitro-Dur contains nicotine

A

false - nitroglycerin

109
Q

name some penetration enhancers for TDDS

A

DMS (decylmethylsulfoxide)
oleic acid
azone
alcohol

110
Q

are pseudoplastic flow and thixotropic flow desirable properties in pharmaceutical suspensions?

A

yes

111
Q

explain a Dilatant

A

a liquid who’s viscosity is increased when stress is applied

as you agitate, viscosity increases

112
Q

in which type of flow are substances called “shear thinning” systems

A

pseduoplastic flow

113
Q

“the flow curve begins at the origin and there is no yield value””

A

pseudoplastic flow

114
Q

true or false

for pseudoplastic flow, the viscosity of the substances increases with increasing shear rate

A

FALSE

Pharmaceutics II Exam 2 (7 decks)

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